Referenced in: none

Automatically associated channels: Kv11.1

Title: Exploring Left-Hand-Side substitutions in the benzoxazinone series of 4-amino-piperidine bacterial type IIa topoisomerase inhibitors.

Authors: Bolin Geng, Janelle Comita-Prevoir, Charles J Eyermann, Folkert Reck, Stewart Fisher

Journal, date & volume: Bioorg. Med. Chem. Lett., 2011 Sep 15 , 21, 5432-5

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/21782427

Abstract
An SAR survey at the C-6 benzoxazinone position of a novel scaffold which inhibits bacterial type IIa topoisomerase demonstrates that a range of small electron donating groups (EDG) and electron withdrawing groups (EWG) are tolerated for antibacterial activity. Cyano was identified as a preferred substituent that affords good antibacterial potency while minimizing hERG cardiac channel activity.